Process for the preparation of .alpha.-6-deoxy- tetracyclines

Details Process for the preparation of .alpha.-6-deoxy- tetracyclines Process for the preparation of .alpha.-6-deoxy- tetracyclines

C - Chemistry, Metallurgy

07

C

260/208.6

C07C 233/00 (2006.01)

Patent

CA 1242704

ABSTRACT A process for the preparation of .alpha.-6-deoxy-tetracyclines by the stereoselective heterogeneous hydrogenation of a 6-demethyl-6-deoxy-6- methylene-tetracycline or an acid addition salt thereof, in the presence of a tertiary phosphine, or the simultaneous dehalogenation and stereo- selective heterogeneous hydrogenation of an 11a-halo-6-demethyl-6-deoxy-6- methylene-tetracycline or an acid addition salt thereof, in the presence of a tertiary phosphine, characterised by the use of a rhodium salt catalyst, wherein the rhodium is bonded to a polysiloxane carrier, having the following formulae: Rh Cl3 [N {(CH2)3 Si O3/2 }3 ]10 Rh Cl3 [N {(CH2)3 Si O3/2 }3 ]12 Rh Cl3 [N {(CH2)3 Si O3/2 }3 ]15 Rh Cl3 [HN{ (CH2)3 Si O3/2} 2] 4 Rh Cl3 [HN{ (CH2)3 Si O3/2} 2] 8 permitting easy recovery of the rhodium, by simple filtration.

461264

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